This invention relates to the use of betulinic acid derivatives for the inhibition and or prevention of cancer growth. The invention also relates to novel betulinic acid derivatives useful for inhibition of tumor or cancer cells and a process for the preparation of the derivatives. The invention also relates to anti-leukemic and anti-lymphoma activity of the betulinic acid derivatives, and the use of the derivatives for the treatment of prostate, lung, laryngeal, colon and ovarian cancer.
The present invention provides for betulinic acid derivatives, methods for preparing betulinic acid derivatives and pharmaceutical compositions comprising betulinic acid derivatives. The derivatives and pharmaceutical compositions comprising betulinic acid derivatives can be used to kill and/or inhibit multiplication of cancer or tumor cells. The bioactivity of the derivatives may be tested using systems normally used by those of skill in the art such as using cultured human leukemia (MOLT-4), lymphoma cells (U937), prostate cancer cells (DU 145), colon cancer cells (HT-29), lung cancer cells (L132), ovarian cancer cells (PA-1) and/or laryngeal cancer cells (HeP.2).
In a preferred embodiment, a pharmaceutically acceptable carrier, diluent, or solvent is used. The invention provides a method of treatment for humans, mammals, or other suffering from cancer or other tumors. The method may suitable comprise, consist of, or consist essentially of administering a therapeutically effective dose of the pharmaceutical composition so as to kill or inhibit the multiplication of cancer or tumor cells. The method of the treatment of the present invention may be particularly useful in the treatment of leukemias and lymphomas and in general in the treatment of prostate, lung, colon and laryngeal cancer.
An object of the invention is to provide a method and composition for inhibiting tumor growth and, particularly, for inhibiting the growth of leukemias and lymphomas and for inhibiting the growth of prostate, colon, larynx, lung and ovarian cancer using betulinic acid, one or more betulinic acid derivatives or a combination thereof.
A further object of the invention is to provide for novel derivatives of betulinic acid and methods for preparing the novel derivatives.
A further object of the invention is to provide a treatment method using betulinic acid derivatives to prevent the growth of cancerous cells, wherein betulinic acid derivative is administered systemically.
A still further object of the invention is to overcome the problem of high toxicity associated with standard chemotherapeutic agents by using a natural product-derived compound, e.g., betulinic acid derivatives.
Yet another object of the invention is to overcome the problem of insufficient availability associated with synthetic anticancer agents by using synthetic derivatives of betulinic acid.
Still another object of the invention is to provide a pharmaceutical formulation containing betulinic acid derivatives, alone or in combination.